English

• 1. [1] S.L. Murphy, J.Q. Xu, K.D. Kochanek, Deaths: final data for 2012, Natl. Vital Stat. Rep. 61 (2013) 1-117.

  2. [2] J.L. Cummings, Alzheimer's disease, N. Engl. J. Med. 351 (2004) 56-67.

  3. [3] V.R. Bennett, S. Kahn, E.A. Mendiaz, et al., Beta-secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE, Science 286 (1999) 735-741.

  4. [4] M. Citron, Emerging Alzheimer's disease therapies: inhibition of β-secretase, Neurobiol. Aging 23 (2002) 1017-1022.

  5. [5] L. Hong, G. Koelsch, X. Lin, et al., Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor, Science 290 (2000) 150-153.

  6. [6] L. Hong, R.T. Turner, G. Koelsch, et al., Crystal structure of memapsin 2 (β-secretase) in complex with an inhibitor OM00-3, Biochemistry 41 (2002) 10963-10967.

  7. [7] J. Liu, W.Y. Chen, Y.C. Xu, et al., Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors, Bioorg. Med. Chem. 23 (2015) 1963-1974.

  8. [8] A.K. Ghosh, M. Brindisi, Y.C. Yen, et al., Structure-based design, synthesis and biological evaluation of novel β-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand, Bioorg. Med. Chem. Lett. 25 (2015) 668-672.

  9. [9] S.Y. Jeon, K.H. Bae, Y.H. Seong, et al., Green tea catechins as a BACE1 (β-secretase) inhibitor, Bioorg. Med. Chem. Lett. 13 (2003) 3905-3908.

  10. [10] T. Kimura, D. Shuto, S. Kasai, et al., KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine, Bioorg Med. Chem. Lett. 14 (2004) 1527-1531.

  11. [11] Y. Cheng, J. Brown, T.C. Judd, et al., An orally available BACE1 inhibitor that affords robust CNS Aβ reduction without cardiovascular liabilities, ACS Med. Chem. Lett. 6 (2015) 210-215.

  12. [12] I.V. Efremov, F.F. Vajdos, K.A. Borzilleri, et al., Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design, J. Med. Chem. 55 (2012) 9069-9088.

  13. [13] J. Tseng, M. Dockendorf, G. Krishna, et al., Safety and pharmacokinetics of the novel BACE inhibitor MK-8931 in healthy subjects following single-and multipledose administration, Alzheimer's Dement. 8 (2012) 184-185.

  14. [14] R. Lai, B. Albala, J.M. Kaplow, et al., First-in-human study of E2609, a novel BACE1 inhibitor, demonstrates prolonged reductions in plasma beta-amyloid levels after single dosing, Alzheimer's Dement. 8 (Supp.) (2012) P96.

  15. [15] K. Höglund, H. Salter, H. Zetterberg, et al., Monitoring the soluble amyloid precursor protein α (SAPPA) and β (SAPPB) fragments in plasma and CSF from healthy individuals treated with BACE inhibitor azd3293 in a multiple ascending dose study: pharmacokinetic and pharmacodynamic correlate, Alzheimer's Dement. 10 (Supp.) (2014) P447.

  16. [16] H. Takahashi, H. Fukumoto, R. Maeda, et al., Ameliorative effects of a noncompetitive BACE1 inhibitor TAK-070 on Aβ peptide levels and impaired learning behavior in aged rats, Brain Res. 1361 (2010) 146-156.

  17. [17] J.K. Liu, W. Gu, X.R. Cheng, et al., Design and synthesis of cyclic acylguanidines as BACE1 inhibitors, Chin. Chem. Lett. 26 (2015) 1327-1330.

  18. [18] S. Geschwindner, J. Ulander, P. Johansson, Ligand binding thermodynamics in drug discovery: still a hot tip? J. Med. Chem. 58 (2015) 6321-6335.

  19. [19] M.S. Malamas, J. Erdei, I. Gunawan, et al., Aminoimidazoles as potent and selective human b-secretase (BACE1) inhibitors, J. Med. Chem. 52 (2009) 6314-6323.

•